CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 uM for TTK and CLK2, respectively.
CC-671 (compound 23) is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 uM for TTK and CLK2, respectively. HCT-116 cell lysates treated with CC-671 at 3 uM for 1 h demonstrates that only four kinases show cellular binding of 75% or more including CLK2, CAMKK2, PIP4K22, and JNK[1].
CC-671 (compound 23) demonstrates significant tumor growth inhibition (TGI) ((vehicle -treated/vehicle) ×100%) of 71% at both 10 and 20 mg/kg on a every 3 days (q3d) dosing schedule. The body weight loss (BWL) in the CC-671 treated group (20 mg/kg ) is higher than in the 10 mg/kg group (17% vs 5%)[1].
References:
[1]. Riggs JR, et al. The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatmentof Triple Negative Breast Cancer Initiated from a Phenotypic Screen. J Med Chem. 2017 Nov 9;60(21):8989-9002.